新型含磷血管紧张素转换酶抑制剂(S)-1-[6-氨基-2[[羟基(4-苯基丁基)膦基]氧]-1-氧己基]- l -脯氨酸(SQ 29,852)对有意识高血压犬的降压作用

N Ohara, M Takizawa, S Yokota, N Ogawa, H Katsumura, H Ono
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引用次数: 2

摘要

研究了含磷新型血管紧张素转换酶抑制剂(S)-1-[6-氨基-2[[羟基(4-苯基丁基)膦]氧]-1-氧己基]- l -脯氨酸(SQ 29,852)对有意识双肾单钳Goldblatt高血压犬的降压效果。比较SQ 29852与卡托普利、依那普利各3mg /kg, p.o的急性降压效果,其效价排序为:依那普利优于SQ 29852,优于卡托普利。另一方面,重复给药SQ 29,852 (3mg /kg, p.o./d,连续7 d,然后再给药10mg /kg, p.o./d,连续7 d)引起的低血压比相同剂量的依那普利更明显。依那普利组所有动物的血尿素氮(BUN)均升高,而SQ 29,852组所有动物的血尿素氮(BUN)均未升高。这些结果表明SQ 29852是一种有效、长效的ACEI,副作用发生率可能较低。
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Hypotensive effect of a phosphorus-containing novel angiotensin converting enzyme inhibitor, (S)-1-[6-amino-2[[hydroxy(4-phenylbutyl)phosphinyl] oxy]-1-oxohexyl]-L-proline (SQ 29,852) in conscious hypertensive dogs.

The hypotensive efficacy of (S)-1-[6-amino-2[[hydroxy(4-phenylbutyl) phosphinyl]oxy]-1-oxohexyl]-L-proline (SQ 29,852), a phosphorus-containing novel angiotensin converting enzyme inhibitor (ACEI) was examined in conscious two-kidney, one-clip Goldblatt hypertensive dogs. The acute hypotensive effect of SQ 29 852 was compared with that of captopril or enalapril at 3 mg/kg, p.o., for each, and the potencies were ranked as follows, enalapril greater than SQ 29,852 greater than captopril. On the other hand, the hypotension caused by repetitive dosing with SQ 29,852 (3 mg/kg, p.o./d for 7 d followed by another 7-d treatment with 10 mg/kg, p.o./d) was somewhat more marked than that by enalapril at the same dosage. Blood urea nitrogen (BUN) increased in all the animals given enalapril, while that in all of the SQ 29,852-treated animals did not increase. These results indicate that SQ 29,852 is a potent, and long-lasting ACEI with a possible low incidence of side effects.

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